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7241756 |
Combinations of dipeptidyl peptidase IV inhibitors and other antidiabetic agents for the treatment of diabetes mellitus
A method for the treatment of diabetes mellitus, especially Type 2 diabetes and conditions associated with diabetes mellitus in a mammal such as a human, which method comprises administering an...
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7112582 |
Bicyclic 6-alkylidene-penems as β-lactamase inhibitors
The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
wherein...
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7094431 |
Method of healing skin wounds in mammals and a composition therefor
This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or...
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7018997 |
Tricyclic 6-alkylidene-penems as β-lactamase inhibitors
The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
wherein...
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6489316 |
6-(spirocyclopropyl) penicillanic acid 4, 4-dioxides
The 6-(spirocyclopropyl)-penicillanic acid 4,4-dioxides of the general Formula (I): as defined herein above which exhibit beta-lactamase inhibiting activity, use of such compounds in combination...
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6472383 |
Pharmaceutical formulations
A pharmaceutical formulation comprises, in combination with a penem of formula (I): in which: R 1 is hydrogen or an organic substituent group; R 2 is a fused bicyclic heterocyclic ring system...
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6426342 |
Use of β-lactamase inhibitors as neuroprotectants
Novel neuroprotectant methods are described. β-Lactamase inhibitors are used to prevent or reduce loss of neuronal cells and neuronal cell function in patients afflicted with or susceptible to...
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6180621 |
Method and treatment using 1-methylcarbapenem derivatives as an anti-helicobacter pylori agent
A method for the prophylaxis or treatment of infectious diseases caused by helicobacter pyloir, by administering a pharmacologically effective amount of a 1-methoylcarbapenem coumpund of formula...
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5945413 |
Aspartyl protease inhibitors
This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of aspartyl protease inhibitors characterized...
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5911985 |
Pharmaceutical formulations containing a β-lactamase inhibiting penem in combination with β-lactam antibiotic and their use in the treatment of bacterial infections
A pharmaceutical formulation comprises, in combination with a penem of formula (I), in which: R 1 is hydrogen or an organic substituent group; R 2 is a fused bicyclic heterocyclic ring system of...
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5637580 |
Antimicrobial penem-quinolones
Compounds of structure: ##STR1## as well as their pharmaceutically-acceptable salts and biohydrolyzables esters, and hydrates thereof, are effective antiinfective agents, useful in treating and...
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5480880 |
Penem derivatives
The invention provides compounds of the general formula I ##STR1## wherein R 1 is a hydrogen atom, a negative charge or an ester residue; R is: a) --(CH 2 ) n --A--CO 2 H, --(CH 2 )n--A--SO 3...
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4876251 |
Tricyclic penam compounds, their production and their use
The compounds, having a 4,10-dioxo-3-oxa-7-thia-1-azatricyclo[6,2,0,0 2 ,6 ]decane-2-carboxylic acid skeleton as the base structure, their esters and their salts, are useful antibacterial agents.
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4826833 |
6-(Substituted)methylene-penicillanic and 6-(substituted)hydroxymethylpenicillanic acids and derivatives thereof
Beta-lactamase inhibiting compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition or carboxylate salt thereof; where n is zero, 1 or 2; X 3 is H or Br, R 1 is H, the...
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4782050 |
6-beta(substituted)-(S)-hydroxymethylpenicillanic acids and derivatives thereof
Antibacterial penicillins of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R 1 is a heterocyclic group and R is hydrogen, the residue of certian carboxy protecting...
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4692441 |
Chorine esters as absorption-enhancing agents for drug delivery through mucous membranes of the nasal, buccal, sublingual and vaginal cavities
Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.
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4650794 |
6-(1-hydroxyethyl)-2-carbamimidoyl-pen-2-em-3-carboxylic acids
Disclosed are 6-(1-hydroxyethyl)-2-carbamimidoyl-pen-2-em-3-carboxylic acids (I) having the representative structure: ##STR1## wherein: A is a direct, single bond connecting the indicated S and C...
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4614737 |
2-dioxacycloalkylthiopenem derivatives
Certain 2-dioxacycloalkylthio-2-penem-3-carboxylic acid compounds are useful as antibacterials for treating mammals and have the formula ##STR1## or a pharmaceutically acceptable salt thereof,...
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4612337 |
Method for preparing infection-resistant materials
An infection-resistant polymeric material, such as polytetrafluoroethylene, for use on or within a human or animal body, for example, in the form of a vascular graft, can be prepared by an improved...
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4582829 |
Antibacterial 6'-(2-amino-2-[4-acyloxyphenyl]acetamido)penicillanoyloxymethyl penicillanate 1,1-dioxide compounds
6-(2-Amino-2-[4-acyloxyphenyl]acetamido)penicillanoyloxymeth
yl esters of penicillanic acid 1,1-dioxide are useful as antibacterial agents. Derivatives of the aforesaid antibacterial agents which...
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4537886 |
β-lactam antibacterial agents and compositions containing them
A compound of formula (1) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R 1 is phenyl, substituted phenyl or a 5- or 6-membered heterocyclic ring...
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4524073 |
β-Lactam compounds
A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R represents an alkyl or aralkyl group, substituted on an alkyl carbon atom...
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4505915 |
6-N-Heterocyclyl penicillins
This invention relates to a new class of penicillins (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics: ##STR1## wherein the stylized radical (hereafter...
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4503040 |
6-(Aminoacyloxymethyl)penicillanic acid 1,1-dioxides as beta-lactamase inhibitors
Beta-lactamase inhibitors which are aminoacid esters of 6-alpha- and 6-beta-(hydroxymethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof...
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4485110 |
β-Lactam compounds, and use
A class of 6-alkylidene penem compounds of formula (II) have antibacterial and β-lactamase inhibitory properties: ##STR1## where R 1 and R 2 represent hydrogen or optionally substituted...
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4462934 |
Bis-esters of dicarboxylic acids with amoxicillin and certain hydroxymethylpenicillanate 1,1-dioxides
Antibacterial bis-esters of 1,4-cyclohexanedicarboxylic acids and alkane dicarboxylic acids wherein the ester moieties are derived from different alcohols; one alcohol being...
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4457924 |
1,1-Alkanediol dicarboxylate linked antibacterial agents
Useful antibacterial agents in which a penicillin and/or a beta-lactamase inhibitor are linked via 1,1-alkanediol dicarboxylates are of the formula ##STR1## where A is the residue of certain...
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4452796 |
6-Aminoalkylpenicillanic acid 1,1-dioxides as beta-lactamase inhibitors
Beta-lactamase inhibitors which are 6-alpha- and 6-beta-(aminomethyl) and (1-aminoethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which...
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4446144 |
Derivatives of penicillanic acid
This invention relates to penicillanic acid derivatives of the formula I ##STR1## in which X stands for chlorine, bromine or iodine, to pharmaceutically acceptable, non-toxic salts of the compounds...
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4432987 |
Crystalline benzenesulfonate salts of sultamicillin
Novel benzenesulfonic acid addition salts of sultamicillin of the formula ##STR1## and hydrated forms thereof, where X is hydrogen or chloro, especially the crystalline dihydrate salts, having...
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4428935 |
Penicillanic acid dioxide prodrug
A compound of the formula ##STR1## is a prodrug of 4,4-dioxopenicillanic acid, wherein R is hydrogen or methyl; R 1 , R 2 and R 3 (a) when taken individually are each alkyl containing one to four...
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4427678 |
6-Aminomethylpenicillanic acid 1,1-dioxide derivatives as beta-lactamase inhibitors
beta-Lactamase inhibitors which are 6-alpha- and 6-beta(aminomethyl)pencillanic acid 1,1-dioxides which are substituted on amino nitrogen with benzyl, hydroxybenzyl, picolyl or phenethyl;...
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4425337 |
Adjuvants for rectal delivery of drug
A method and drug form enhancing the rate of absorption of a rectally administered drug from the rectal compartment into the blood stream of a warm blooded animal. The method includes the steps of...
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4416880 |
β-Lactam antibiotics and compositions containing the same
β-Lactam antibiotics of the formula ##STR1## in which A is a hydrogen atom, an optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl group, a substituted or unsubstituted phenyl ring, a...
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4382089 |
Antibacterial amide compounds, compositions thereof and methods of using them
Novel organic amide compounds which are N-[[(acylaminoacylamino or aminoacylamino9]-dihydro-oxo-3-quinolinylcarbonyl]penicillin
compounds having broad spectrum antibacterial utility are provided...
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4377590 |
Derivatives of ampicillin and amoxicillin with beta-lactamase inhibitors
Certain beta-lactamase inhibitors which have a beta-lactam ring as well as a carboxy group have been linked through their carboxy group to either the amino group of ampicillin, the amino group of...
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4376767 |
Pyridylmethyl esters of selected bio-affecting carboxylic acids
Novel pharmaceutically useful derivatives of selected known bio-affecting carboxylic acids are disclosed, said derivatives having the structural formula ##STR1## wherein R 1 and R 2 , which can be...
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4375434 |
Process for 6'-amino-penicillanoyloxymethyl penicillanate 1,1-dioxide
6'-Aminopenicillanoyloxymethyl penicillanate 1,1-dioxide is prepared by a two-step procedure. The first step consists of coupling a salt of a 6-(protected amino)penicillanic acid with a halomethyl,...
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4364957 |
Bis-esters of alkanediols as antibacterial agents
6-Acylaminopenicillanoyloxymethyl esters and 1-(6-acylaminopenicillanoyloxy)ethyl esters of 2-beta-acetoxymethyl-2-alpha-methyl-(5R)penam-3-alpha-carbox
ylic acid 1,1-dioxide are useful as...
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4359472 |
Bis-hydroxymethyl carbonate bridged antibacterial agents
Antibacterial agents in which a penicillin and a beta-lactamase inhibitor are linked by means of a bis-hydroxymethyl carbonate bridge are of the formula: ##STR1## and pharmaceutically acceptable...
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4356174 |
Beta-lactamase inhibiting 2-beta-substituted-2-alpha-methyl-(5R)penam-3-alpha-carboxylic acid 1,1-dioxides and intermediates therefor
Beta-lactamase inhibiting 2-beta-substituted-2-alpha-methyl-(5R)penam-3-alpha-carboxyl
ic acid 1,1-dioxides and esters thereof, wherein the 2-beta-substituent is cyano, acetyl, alkoxycarbonyl,...
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4352800 |
Adjuvant for promoting absorption of therapeutically active substances through the digestive tract
The enamine derivatives having following formula ##STR1## promote absorption of therapeutically active substances through the digestive tract into the blood stream and are able to effectively...
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4351840 |
Antibacterial esters of resorcinol with ampicillin and penicillanic acid 1,1-dioxide derivatives
Bis-esters of resorcinol (1,3-dihydroxybenzene) with ampicillin or amoxicillin and penicillanic acid 1,1-dioxide or 6-beta-(hydroxymethyl)penicillanic acid 1,1-dioxide, having utility as...
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4342772 |
β-Lactam compounds, antibacterial compositions thereof and method of use
The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R 1 stands for a phenyl, 4-hydroxyphenyl, 1,4-cyclohexadienyl or a 3-thienyl group; R 2 ...
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4320133 |
Penicillins and their antibacterial use
The invention provides novel penicillins and cephalosporins of formula I, ##STR1## methods for their production and their anti-bacterial use.
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4317820 |
β-Lactam series compound and antibacterial pharmaceutical composition containing the same
A β-lactam series compound represented by the formula (I): ##STR1## wherein R 1 represents a hydrogen atom or a lower alkyl group; R 2 represents a hydrogen atom; R 3 represents a halogen atom,...
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4303664 |
Novel penicillin derivatives containing a coumarin nucleus and medicines containing the same
This invention provides novel penicillin derivatives of formula [I]; ##STR1## wherein A is hydrogen or hydroxyl, and B represents the cumarin nucleus of formula [III-a]; ##STR2## in which B 1 , B 2...
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4293560 |
Talampicillin 2-methoxyphenoxyacetate and pharmaceutical compositions containing it
Talampicillin 2-methoxyphenoxyacetate; a process for its preparation by acid hydrolysis of the metampicillin phthalidyl ester in a biphasic aqueous-organic solvent and treatment of the resulting...
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4283402 |
6-N-Heterocyclyl-3-tetrazolyl-penicillins
This invention relates to a new class of penicillins (I) and their pharmaceutically acceptable salts which are useful as antibiotics: ##STR1## wherein the stylized radical (hereafter referred to as...
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4282236 |
β-Lactam antibacterial agents, their use in pharmaceutical compositions, and intermediates
The compounds of the formula (II): ##STR1## and salts and cleavable esters thereof wherein R 1 is a hydrogen atom or a lower alkyl group and R 2 is a CN or CO 2 R 3 group where R 3 is a...
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